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Necrosulfonamide

Catalog No. T6904 CAS 1360614-48-7

Synonyms: (E)-Necrosulfonamide

(E)-Necrosulfonamide is an inhibitor of necroptosis. Blocks mixed lineage kinase domain-like protein (MLKL), a critical substrate of receptor-interacting serine-threonine kinase 3 (RIP3) during necrosis. Prevents MLKL-RIP1-RIP3 necrosome complex from interacting with downstream necrosis effectors. Binds and inhibits gasdermin D. Inhibits pyroptosis.

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Necrosulfonamide, CAS 1360614-48-7

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	(E)-Necrosulfonamide is an inhibitor of necroptosis. Blocks mixed lineage kinase domain-like protein (MLKL), a critical substrate of receptor-interacting serine-threonine kinase 3 (RIP3) during necrosis. Prevents MLKL-RIP1-RIP3 necrosome complex from interacting with downstream necrosis effectors. Binds and inhibits gasdermin D. Inhibits pyroptosis.
In vitro	Necrosulfonamide inhibits MLKL-mediated Necrosis by blocking its N-terminal CC domain function. It blocks necrosis downstream of RIP3 activation. Necrosulfonamide has no effect on apoptosis induced by TNF-α plus Smac mimetic in non-RIP3-expressing Panc-1 cells, even at 5 μM concentration. Necrosulfonamide efficiently blocks necrosis in human cells, but not mouse cells. The reason for the species specificity of necrosulfonamide is that the cysteine at residue 86 in human MLKL that is covalently modified by necrosulfonamide is replaced by a tryptophan residue in mouse MLKL(mixed lineage kinase domain-like protein)[2].
Kinase Assay	PRMT Biochemical Assays: A scintillation proximity assay (SPA) is used for assessing the effect of test compounds on inhibiting the methyl transfer reaction catalyzed by PRMTs. In brief, the tritiated S-adenosyl-L-methionine (3H-SAM) is used as the donor of methyl group. The (3H) methylated biotin labeled peptide is captured in a streptavidin/scintillant-coated microplate, which brings the incorporated 3H-methyl and the scintillant to close proximity resulting in light emission that is quantified by tracing the radioactivity signal (counts per minute) as measured by a TopCount NXT Microplate Scintillation and Luminescence Counter. When necessary, nontritiated SAM is used to supplement the reactions. The IC50 values are determined under balanced conditions at Km concentrations of both substrate and cofactor by titration of test compounds in the reaction mixture.
Cell Research	Necrosis inhibitors induce diverse effects on MLKL phosphorylation. HT-29 cells are treated with T/S/Z with or without necrosis inhibitors for 12 hr or 8 hr. The number of dead cells is determined by measuring released protease activity in culture medium. The whole-cell extracts are prepared and analyzed by western blotting. The final concentrations of 10 μM necrostatin-1 or 1 μM necrosulfonamide are used to block necrosis. (Only for Reference)

Synonyms	(E)-Necrosulfonamide
Molecular Weight	461.47
Formula	C18H15N5O6S2
CAS No.	1360614-48-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 9.2 mg/mL (20 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Daohong Liao, et al. Med Chem Commun. 2014, 5, 333. 2. Sun L, et al. Cell. 2012, 148(1-2):213-27. 3. Wang H, et al. Mol Cell. 2014, 54(1):133-46. 4. Teng J F, Mei Q B, Zhou X G, et al. Polyphyllin VI Induces Caspase-1-Mediated Pyroptosis via the Induction of ROS/NF-κB/NLRP3/GSDMD Signal Axis in Non-Small Cell Lung Cancer[J]. MLA . Cancers. 2020, 12(1): 193. 6. Zhang J, Zhou B, Sun R, et al. The metabolite α-KG induces GSDMC-dependent pyroptosis through death receptor 6-activated caspase-8[J]. Cell Research. 2021: 1-18.

Citations

1. Zhang J, Zhou B, Sun R, et al. The metabolite α-KG induces GSDMC-dependent pyroptosis through death receptor 6-activated caspase-8. Cell Research. 2021: 1-18. 2. Yang W, Liu S, Li Y, et al. Pyridoxine induces monocyte-macrophages death as specific treatment of acute myeloid leukemia. Cancer Letters. 2020 3. Teng J F, Mei Q B, Zhou X G, et al. Polyphyllin VI Induces Caspase-1-Mediated Pyroptosis via the Induction of ROS/NF-κB/NLRP3/GSDMD Signal Axis in Non-Small Cell Lung Cancer MLA. Cancers. 2020, 12(1): 193.

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Keywords

Necrosulfonamide 1360614-48-7 MAPK MLK formation (E)-Necrosulfonamide necrosis necrosome substrate RIP3 Inhibitor inhibit complex Mixed Lineage Kinase MLKs inhibitor

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